2-Chlorobenzoyl hydrazine refluxed with benzoyl isothiocyanate and phenyl isothiocyanate in ethanol for 3 hours to give benzamide derivative (1) and anilinederivative (2) on yield of 71%and 95%, respectively. Benzamide derivative (1) reacted with ethanolic sodium hydroxide on reflux to afford cyclization product (3), followed by general substitution reaction of two steps to give acetamide (5), and derivatived acetamides 7a-7k, while aniline derivative (2) reacted with ethanolic sodium hydroxide on reflux to afford another cyclization product (4). Thiol (4) reacted with N-phenyl chloroacetamide in the presence of potassim carbonate to give acetamide derivative (6). Compounds 1-7kwere evaluated for their growth inhibition against five cancer cell lines, including human lung carcinoma (A-549), human prostate cancer (DU145), human colon adenocarcinoma (HT-29), human malignant melanoma (SK-MEL-2) and human ovary malignant ascites (SK-OV-3) with sulforhodamine B (SRB) assay. All compounds (1-7k) showed low inhibition activities under 50% on 100M concentration.

[1,2,4]-Triazole derivatives were synthesized by 5 steps. Benzimidazole was refluxed with ethyl chloroacetate to give 1H-benzimidazole-acetic acid ethyl ester (1) over 52% yield. Ester (1) was refluxed with hydrazine hydrate in the presence of ethanol to afford 1H-benzimidazole-1-acetic acid, hydrazide (2). 5-Benzoimidazol-1-ylmethyl-4H-[1,2,4]triazole-3-thiol (4) was made via coupling of compound (2) with methyl isothiocyanate, followed by cyclization of 1H-benzimidazole-1-acetic acid, 2-[(methylamino) thioxomethyl]hydrazide (3) on reflux, and finally the target compounds (6a-6v) were synthesized by general substitution reaction. Compounds (6a-6v) were screened for T-type calcium channel blocker using the fluorescence assay by FDSS6000. All compounds (6a-6v) did not show better activities than control compound, mibefradil.